Abstract: The present invention provides a process for the synthesis of olopatadine. Further, the invention discloses a process that results in improved yield of the desired Z isomer.

Abstract: The present invention relates to glioblastoma inhibiting compounds, in particular gambogic acid amid and derivatives thereof for the treatment of glioblastoma. Moreover, methods for determining whether a treatment with the compounds of the invention is suitable for a patient are disclosed.

Abstract: Olopatadine can be obtained by means of a process comprising hydrolysis of a compound of general formula (II), wherein Y is OR1, wherein R1 is C1-C7 alkyl, C3-C7 cycloalkyl, aryl, arylalkyl, or heterocycle; or NR2R3, wherein R2 and R3, independently from each other, are C1-C7 alkyl, aryl, arylalkyl, or R2 and R3 together with the nitrogen atom to which they are bound form a heterocycle of 3 to 7 members, obtained by means of a process comprising reacting the corresponding ester or amide of 6,11-dihydro-11-oxodibenz[b,e]oxepin-2-acetic acid with a suitable Wittig reagent, in the presence of a base in a reaction medium comprising an organic solvent.

Abstract: A process for the preparation of olopatadine hydrochloride starting from an advanced intermediate.

Abstract: Disclosed are a new method for synthesizing 7-membered fused heterocycles and compounds synthesized by the new method. The method involves a dual activation strategy using an N-heterocyclic carbene catalyst as a first Lewis base and another second Lewis base. Compounds synthesized by the disclosed method may include new benzoxopinone compounds, as well as benzoxepane compounds and benzoazepinone compounds that optionally may be derived from the disclosed benzoxopinone compounds.

Abstract: Monomeric and dimeric trioxane thioacetals and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.

Abstract: The invention relates to compounds from the soft coral and the generation thereof. The invention also relates to the uses of the compounds from the soft coral in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2.

Abstract: The present invention relates to a novel process for the preparation of olopatadine hydrochloride starting from an advanced intermediate.

Abstract: Process for the preparation of intermediates that are useful in the synthesis of active pharmaceutical ingredients (API), in particular active in the central nervous system.

Abstract: Store operated calcium channel modulating compounds, and methods for using the same, are provided. These compounds and methods find use in a variety of applications in which modulation of store operated calcium channels is desired.

Abstract: The present invention provides a method for treating a patient having cancer comprising administering to the patient a therapeutically effective amount of compound (1), or a pharmaceutically acceptable salt thereof, having the formula: The present invention also provides a kit containing the above compound.

Abstract: Fullerene?CTV complexes, comprising fullerene?CTV hemicarceplexes, formed by various cyclotriveratrylene (CTV)-based molecular cages and various fullerene guests are disclosed. A method of direct isolating at least a fullerene from fullerene mixtures by using the above fullerene CTV hemicarceplexes but without using crystallization or HPLC is also disclosed.

Abstract: The invention relates to doxepin, pharmaceutically acceptable salts and prodrugs of doxepin; compositions containing the same, and the use of any of the aforementioned for the treatment of sleep disorders.

Abstract: Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.

Abstract: The invention relates to compounds of formula (?) as further defined herein and to the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to the uses thereof. The compounds and salts of the present invention inhibit anaplastic lymphoma kinase (ALK) and/or EML4-ALK and are useful for treating or ameliorating abnormal cell proliferative disorders, such as cancer.

Abstract: Disclosed are compounds that are conjugates of ladder frame polyether compounds and biologically active compounds or research compounds, pharmaceutical formulations comprising the conjugates, and methods of transporting the conjugates across biological membranes.

Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.

Abstract: An aminopropylidene derivative having excellent histamine receptor antagonistic action, a compound which is useful as a pharmaceutical composition, especially as an active ingredient, having alleviated side effects in the central nervous system is described. In the aminopropylidene derivative, R1 and R2, which may be identical or different, stand for a hydrogen, a substituted carbonyl, a substituted carbonylalkyl, and acrylic acid, excluding a case where both are hydrogen; R3 and R4, which may be identical or different, stand for hydrogen, an alkyl which may be substituted with phenyl, or the like; A stands for unsubstituted or an oxo; B stands for a carbon or an oxygen; one of X and Y stands for a carbon and the other stands for a sulfur, a broken line part stands for a single bond or a double bond, and a wavy line stands for cis-form and/or trans-form.

Abstract: The present invention is directed to novel compounds of formula (I) as well as to the process for their preparation. Novel compounds of formula (I) can be converted into asenapine through an efficient process. The invention also relates to novel intermediates used in this process and their use in the preparation of compounds of formula (I).

Abstract: A process for the preparation of olopatadine hydrochloride starting from an advanced intermediate.

Abstract: A class of compounds useful in pharmaceutical compositions and methods for treating or preventing cancer is described. The compounds' ability to inhibit RET kinase is quantified, i.e., their respective RET IC50 and EC50 values are described. One such compound, known as cyclobenzaprine and herein as SW-01, has been identified as RET-specific with an IC50 of 300 nM. SW-01 inhibits RET autophosphorylation and blocks the growth and transformation of thyroid cancer cell lines. It has been further tested in pancreatic cancer, breast cancer, and SCLC cell lines. The compounds show utility for inhibition of survival and proliferation of tumor cells.

Abstract: Desmethyldoxepin, isomers of desmethyldoxepin, and pharmaceutically acceptable salts and prodrugs of desmethyldoxepin; compositions containing the same, and the use of any of the aforementioned for the treatment of sleep disorders.

Abstract: Cyclic alkynes (e.g., cyclooctynes such as dibenzocyclooctynes) can be photochemically generated from cyclopropenones as disclosed herein. The cyclic alkynes can be reacted (e.g., in situ) with materials having alkyne-reactive groups (e.g., azide groups in a “click” reaction). In preferred embodiments, the generation and reaction of the cyclic alkyne can proceed in the absence of a catalyst (e.g., Cu(I)). These reactions can be useful, for example, for the selective labeling of living cells that are metabolically modified with azido-containing surface monosaccharides, or for light-directed surface patterning.

Abstract: The present invention is directed to novel compounds of formula (I) as well as to the process for their preparation. Novel compounds of formula (I) can be converted into asenapine through an efficient process. The invention also relates to novel intermediates used in this process and their use in the preparation of compounds of formula (I).

Abstract: Methods of preventing early awakenings, and improving sleep efficiency in hours 7 and 8 of a period of sleep, by administration of low doses of doxepin (e.g., 1-6 mg).

Abstract: The present invention relates to a field of pharmaceutical chemistry, more specifically, the present invention relates to a garcinia derivative Formula (I), its preparing method, and medicinal use. Wherein the definitions of R1 and R2 are disclosed in the specification of the present invention, and the derivative of the present invention is a structurally simplified analogue of the gambogic acid compound; wherein the gambogic acid compound possesses anti-cancer characteristics, and could be used for preparation of anti-tumor drugs.

Abstract: Provided is a tricyclic compound having a PPAR ? agonist activity, which is represented by the general formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R4-R9 are the same or different and each represents hydrogen or the like, V represents a single bond or the like, R10 and R11 are the same or different and each represents hydrogen or the like, or a pharmaceutically acceptable salt thereof or the like:

Abstract: Cyclic alkynes (e.g., cyclooctynes such as dibenzocyclooctynes) can be photochemically generated from cyclopropenones as disclosed herein. The cyclic alkynes can be reacted (e.g., in situ) with materials having alkyne-reactive groups (e.g., azide groups in a “click” reaction). In preferred embodiments, the generation and reaction of the cyclic alkyne can proceed in the absence of a catalyst (e.g., Cu(I)). These reactions can be useful, for example, for the selective labeling of living cells that are metabolically modified with azido-containing surface monosaccharides, or for light-directed surface patterning.

Abstract: The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.

Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract: The present invention relates to branched polyethyleneglycol (PEG) derivatives consisting of a molecule with a quaternary carbon connected to three PEG chains, wherein all three PEG chains are of equal length and each comprises 1-30 —OCH2CH2— units, and one group with at least one carbon atom, wherein said at least one carbon atom is attached to the quaternary carbon. Also compositions containing such derivatives and use of such derivatives are disclosed.

Abstract: Cyclic alkynes (e.g., cyclooctynes such as dibenzocyclooctynes) can be photochemically generated from cyclopropenones as disclosed herein. The cyclic alkynes can be reacted (e.g., in situ) with materials having alkyne-reactive groups (e.g., azide groups in a “click” reaction). In preferred embodiments, the generation and reaction of the cyclic alkyne can proceed in the absence of a catalyst (e.g., Cu(I)). These reactions can be useful, for example, for the selective labeling of living cells that are metabolically modified with azido-containing surface monosaccharides, or for light-directed surface patterning.

Abstract: The present invention relates to the use of a compound with the following chemical structure: for the preparation of a medicament, preferably designed for the prevention or treatment of pathological processes related to the tau and ?-amyloid proteins. Preferably, the compound used is gambierol.

Abstract: The present invention refers to the use of a compound with the chemical structure for the preparation of a medicinal drug, preferably for the prevention or the treatment of pathological processes related to the tau and ?-amyloid proteins. The compound preferably used is gymnodimine.

Abstract: The present invention relates to dimeric derivatives of 10-trifluoromethylated artemisinin of formula (I): or a pharmaceutically acceptable salt thereof with B1 and B2 selected from C?O, CHOH and CH2, as well as to their use in treating cancer and to their preparation method.

Abstract: The present invention discloses certain derivatives of artemisinin and the active principles contained in Artemisia annua extracts with amino acids, peptides, and amino sugars and salts thereof (formula I).

Abstract: The present invention discloses certain derivatives of artemisinin and the active principles contained in Artemisia annua extracts with amino acids, peptides, and amino sugars, and isomers and salts thereof (formula I).

Abstract: Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.

Abstract: A compound of formula (I) is described; wherein the substituents are as defined in the text and wherein the compound is intended for use in the production of a vascular damaging effect in a warm-blooded animal.

Abstract: The present invention relates to compounds of the formula I wherein R1, R2, R3, R4, X and Y have the meanings given in the description. The compounds have an action which is immunomodulating and inhibits or regulates the release of IL-1? and/or TNF-?. They can therefore be used for treatment of diseases connected with a disturbance in the immune system.

Abstract: Fluorinated compounds and methods of making fluorinated compounds are described herein.

Abstract: A monomer having the general formula: in which R1 is any substitution; R2 is any substitution; R1 and R2 may be linked to form a saturated or unsaturated ring; L represents a reactive leaving group; X and Y each independently represent CR2, O, BR, NR, SiR2, S, S?O, SO2, PR or P?O(R) wherein R in each occurrence is independently selected from H or a substituent; Z represents a single bond or a divalent atom or group, wherein X—Z—Y forms an unconjugated ring or chain, with the proviso that at least one of R1 and R2 is an aryl or heteroaryl group if Z is a single bond.

Abstract: Disclosed are compounds that are conjugates of ladder frame polyether compounds and biologically active compounds or research compounds, pharmaceutical formulations comprising the conjugates, and methods of transporting the conjugates across biological membranes.

Abstract: The invention relates to compounds from the soft coral and the generation thereof. The invention also relates to the uses of the compounds from the soft coral in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2.

Abstract: The present invention relates to a field of pharmaceutical chemistry, more specifically, the present invention relates to a garcinia derivative Formula (I), its preparing method, and medicinal use. Wherein the definitions of R1 and R2 are disclosed in the specification of the present invention, and the derivative of the present invention is a structurally simplified analogue of the gambogic acid compound; wherein the gambogic acid compound possesses anti-cancer characteristics, and could be used for preparation of anti-tumor drugs.

Abstract: This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.

Abstract: The present invention relates to a process for the preparation of olopatadine and, more particularly, to an improved method of synthesizing olopatadine which comprises reacting a dibenz[b,e]oxepin-11-one derivative of formula (III) and a suitable reagent under Witting condition, and to the intermediate 11-[(Z)-3-(dimethylamino)-propylidene]-6-11-dihydrodibenz[b,e]-oxepin-2-acet-amide p-toluensulfonate salt.

Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.

Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.